Boron Containing Patents (Class 546/13)
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Publication number: 20020137934Abstract: A new ligands that include a benzene ring in the backbone can be combined with a metal or metal precursor compound or formed into a metal-ligand complex catalyze a number of different chemical transformations, including olefin polymerization reactions. The ligands, complexes formed with the ligands and compositions including the ligands are useful catalysts, depending on the reaction.Type: ApplicationFiled: September 18, 2001Publication date: September 26, 2002Applicant: Symyx TechnologiesInventors: Anil Guram, Cheryl Lund, Howard W. Turner, Tetsuo Uno
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Patent number: 6436961Abstract: The present invention relates to a novel process for preparing and resolving 3-amino-2-phenylpiperidine and for synthesizing from the enantiomers of such compound certain pharmaceutically active substituted 2-phenyl-3-benzylaminopiperidines. The substituted 2-phenyl-3-benzylaminopiperidines that can be prepared by the processes of this invention are substance P receptor antagonists and are useful in the treatment and prevention of inflammatory and central nervous system disorders, as well as several other disorders.Type: GrantFiled: September 18, 1995Date of Patent: August 20, 2002Assignee: Pfizer INCInventors: Harry A. Watson, Jr., William M. Snyder, Glenn E. Wilcox
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Patent number: 6410505Abstract: A class of predominantly hydrophilic 1,8-naphthalimide dyes. The dye contains at least two 1,8-naphthalimide ring systems, joined by a spacer moiety. Each of the 1,8-naphthalimide ring system has a ring nitrogen atom and bears, at the 4 position, an amino nitrogen atom, carrying a hydrogen. The remaining unsatisfied valences, if present, of the ring nitrogen atoms or the amino nitrogen atoms, or all, are occupied by one or more alkyl substituents. Each of the 1,8-naphthalimide ring system is free of an azo substituent and is also free of a nucleofuge. Upon activation by an activating agent in an environment independent of the presence or absence of oxygen, these compounds generate activated species. The activated species can cause structural changes in lipid and any associated proteins and polypeptides, extra- or intra-cellular or transmembrane, leading to polymerization and crosslinking.Type: GrantFiled: June 28, 1999Date of Patent: June 25, 2002Assignee: Microbiomed Corp.Inventors: David E. Lewis, Ronald E. Utecht, Millard M. Judy, J. Lester Matthews
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Patent number: 6387992Abstract: Compounds of formula I or II where R is a heteroaryl moiety, such as 3-pyridyl, or T is a heteroaryl moiety, such as thien-2,5-diyl, and E1 and E2 are independently hydrogen, alkyl, aralkyl and the like, are prepared by reaction of a benzotriazole substituted on the 5-position of the benzo ring by a halogen atom with a heteroarylboronic acid or ester in the presence of a transition-metal catalyst, such as palladium (II) diacetate. The benzotriazole compounds of formula I are particularly efficacious as stabilizers for automotive coatings and candle wax.Type: GrantFiled: November 27, 2000Date of Patent: May 14, 2002Assignee: Ciba Specialty Chemicals CorporationInventors: Stephen D. Pastor, Anthony DeBellis, Mervin G. Wood, Joseph Suhadolnik, Deborah DeHessa, Ramanathan Ravichandran
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Publication number: 20020052522Abstract: This invention relates to a diboron derivative of formula (I) or a diboron derivative of formula (II) or a diboron derivative of formula (III) where R1, R2, R3 and R4 are each independently selected from the group consisting of optionally substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted cycloalkyl, optionally substituted cycloalkenyl, a group of the formula —(R5Q)mR6 where Q is selected from O, S, NR7, optionally substituted arylene and optionally substituted cycloalkylene, m is an integer selected from 1 to 3, the or and each R5 is independently an optionally substituted C1-C3 alkylene, R6 is C1-C3 alkyl or hydrogen, and R7 is hydrogen or C1-C12 alkyl; each X is independently selected from O, S(O)n and NR7, where n is an integer from 0 to 3, R7 is hydrogen or C1-C12 alkyl, or one or more of —NR1R7, —NR2R7, —NR3R7 and -NR4R7 represent an optionally substituted 5 or 6 membered heterocyclyl group,and A, A1 and A2 are divalent groups wType: ApplicationFiled: October 22, 2001Publication date: May 2, 2002Applicant: Commonwealth Scientific and Industrial Research OrganisationInventors: Sebastian Mario Marcuccio, Mary Rodopoulos, Helmut Weigold
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Patent number: 6376669Abstract: Dye labeled imidazonaphthyridine, imidazopyridine and imidazoquinoline compounds having immune response modulating activity are disclosed. The compounds are useful, inter alia, for determining the binding and/or receptor sites of the molecules.Type: GrantFiled: November 2, 2000Date of Patent: April 23, 2002Assignee: 3M Innovative Properties CompanyInventors: Michael J. Rice, Mark A. Tomai, Ai-Ping Wei
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Patent number: 6369080Abstract: Novel compounds of formula I: including its pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating conditions in mammals characterized by undesired thrombosis.Type: GrantFiled: October 10, 1997Date of Patent: April 9, 2002Assignee: COR Therapeutics, Inc.Inventors: Bing-Yan Zhu, Robert M. Scarborough
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Patent number: 6369224Abstract: A compound of formula wherein n is 0 or 1; m is 0 or 1; p is 0 or 1; X is oxygen or sulfur; Y is CH, N or NO; W is oxygen, H2 or F2; A is N or C(R2); G is N or C(R3); D is N or C(R4); with the proviso that no more than one of A, G, and D is nitrogen, but at least one of Y, A, G, and D is nitrogen or NO; R1 is hydrogen or C1 to C4 alkyl; R2, R3, and R4 are independently hydrogen, halogen, C1-C4 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, aryl, heteroaryl, OH, OC1-C4 alkyl, CO2R1, —CN, —NO2, —NR5R6, —CF3, —OSO2CF3 or R2 and R3, or R3 and R4, respectively, may together form another six membered aromatic or heteroaromatic ring sharing A and G, or G and D, respectively, containing between zero and two nitrogen atoms, and substituted with one to two of the following substituents: independently hydrogen, halogen, C1-C4 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, aryl, heteroaryl, OH, OC1-C4 alkyl, CO2R1, —CN, —NO2, —NR5R6, —CF3, —OSO2CF3; R5 and R6Type: GrantFiled: June 16, 2000Date of Patent: April 9, 2002Assignee: Astra Zeneca ABInventors: Eifion Phillips, Robert Mack, John Macor, Simon Semus
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Patent number: 6368395Abstract: The present invention is directed to methods of making subphthalocyanine compounds. The methods of the present invention may be used to produce known subphthalocyanine compounds, as well as, a new family of subphthalocyanine compounds. The methods of the present invention may employ environmentally-friendly solvents, which donate a hydrogen atom for use in the reaction mechanism. The methods of the present invention produce subphthalocyanine compounds at a yield of greater than about 50%, and even greater than about 94%. The present invention is further directed to subphthalocyanine compounds having improved lightfastness. The subphthalocyanine compounds may have a Subphth-Lightfastness Test Value of less than 15%.Type: GrantFiled: May 12, 2000Date of Patent: April 9, 2002Assignee: Kimberly-Clark Worldwide, Inc.Inventors: Ronald Sinclair Nohr, John G. MacDonald
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Publication number: 20020028351Abstract: The invention provides heterocyclic organoaluminum and organoboron coordination complexes that are photoluminescent and electroluminescent, emitting intense blue light. The invention further provides methods of synthesizing such compounds, methods of producing photoluminescence and electroluminescence, methods of applying the compounds in thin films, and uses of the compounds of the invention in luminescent probes, electroluminescent displays and the like.Type: ApplicationFiled: October 18, 2001Publication date: March 7, 2002Inventors: Suning Wang, Wang Liu, Abdi Hassan
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Publication number: 20020010279Abstract: The present invention provides formulae for fluorescent compounds that have a number of properties which make them uniquely suited for use in sensors of analytes such as saccharides. The advantageous fluorescent properties include favorable excitation wavelengths, emission wavelengths, fluorescence lifetimes, and photostability. Additional advantageous properties include enhanced aqueous solubility, as well as temperature and pH sensitivity. The compound comprises an aryl or a substituted phenyl botonic acid that acts as a substrate recognition component, a fluorescence switch component, and a fluorophore. Fluorescent compounds are described that are excited at wavelengths greater than 400 nm and emit at wavelengths greater than 450 nm, which is advantageous for optical transmission through skin. The fluorophore is typically selected from transition metal-ligand complexes and thiazine, oxazine, oxazone, or oxazine-one as well as anthracene compounds.Type: ApplicationFiled: March 30, 2001Publication date: January 24, 2002Inventors: Joe H. Satcher, Stephen M. Lane, Christopher B. Darrow, Douglas R. Cary, Joe Anh Tran
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Publication number: 20020008465Abstract: An organic boron compound effective for constituting a functional layer in an organic luminescence device is represented by formula (1) below: 1Type: ApplicationFiled: March 28, 2001Publication date: January 24, 2002Inventors: Kazunori Ueno, Koichi Suzuki, Akihiro Senoo, Hiroshi Tanabe, Seiichi Yogi
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Patent number: 6312835Abstract: Heterocyclic organoaluminum and organoboron coordination complexes that are photoluminescent and electroluminescent, emitting intense blue light. Methods of synthesizing such compounds, methods of producing photoluminescence and electroluminescence, methods of applying the compounds in thin films, and uses of the compounds of the invention in luminescent probes, electroluminescent displays and the like.Type: GrantFiled: February 12, 1998Date of Patent: November 6, 2001Assignee: Queen's University at KingstonInventors: Suning Wang, Wang Liu, Abdi Hassan
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Publication number: 20010020033Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: ApplicationFiled: October 10, 1997Publication date: September 6, 2001Inventors: BING-YAN ZHU, ROBERT M. SCARBOROUGH
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Publication number: 20010018429Abstract: The present invention provides bicyclic metabotropic glutamate receptor ligands, as well as compositions comprising such ligands, and and methods for their use.Type: ApplicationFiled: January 25, 2001Publication date: August 30, 2001Inventors: Alan P. Kozikowski, Darryl Hugh Steensma, Werner Tueckmantel, Gian Luca Araldi
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Patent number: 6281154Abstract: Novel compounds having one group 13 element bound with one mono- or di-anionic tridentate ligand, a method of preparation thereof and use thereof as a copolymerization catalyst.Type: GrantFiled: October 28, 1998Date of Patent: August 28, 2001Assignees: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S), Centre National de la Recherche Scientifique (CNRS)Inventors: Guy Bertrand, Jean Bernard Cazaux, Norbert Emig, RĂ©gis Reau
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Publication number: 20010014739Abstract: Tetrakis(fluoroaryl)borate•magnesium halide (Ar4BMgX) expressed by General Formula (1): 1Type: ApplicationFiled: February 9, 2001Publication date: August 16, 2001Applicant: NIPPON SHOKUBAI CO., LTD.Inventors: Hitoshi Mitsui, Tsunemasa Ueno, Ikuyo Ikeno, Naoko Yamamoto
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Patent number: 6252082Abstract: The invention concerns compounds of formula (I) in which: R is —NO2 or —NHR3, R3 being hydrogen, —COR4 (R4 selected among (C1-C4) alkyl, aryl and aryl (C1-C4) alkyl, —COOR5 (R5 selected among (C1-C4) alkyl and aryl (C1-C4) alkyl), —CONHR6 or SO2R6 (R6 selected among (C1-C5) alkyl, aryl and aryl(C1-C4) alkyl), —SO2NR7R8 (R7 and R8 independently of each other represent hydrogen or (C1-C4) alkyl or form with the nitrogen atom a morpholine group), aryl (C1-C4) alkyl, R1 is a (C1-C4) alkyl group linear or branched, cyclo (C3-C8) alkyl, aryl optionally substituted, aryl (C1-C4) alkyl optionally substituted, heteroaryl, R2 is a hydrogen atom, a (C1-C4) alkyl or arylmethyl group, X is an oxygen or sulphur atom, a —CH2—, —SO2 or —NR1— group and Y is a hydrogen atom or (C1-C6) alkyl. The invention is applicable to synthesis intermediates.Type: GrantFiled: July 14, 1999Date of Patent: June 26, 2001Assignee: Sanofi-SynthelaboInventors: Gilbert Lassalle, Patrice Bellevergue, Jean-Claude Bourbier, Daniel Galtier, ValĂ©rie Martin
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Patent number: 6179937Abstract: The stability of HAN, HAN derivatives or hydroxylamine, and compositions comprising these is considerably enhanced by employing a stabilizing effective amount of a stabilizer selected from (a) a pyridine or pyridone salt, or an acid thereof; (b) a diphosphonate or methylenephosphonate salt, or an acid thereof; or (c) a mixture of two or more stabilizers, wherein at least one is selected from (a) and at least one is selected from (b). Stabilized HAN, HAN derivatives, or hydroxylamine or compositions comprising HAN, an HAN derivative or hydroxylamine, along with a process for providing these stabilized compositions is described. A stabilizer mixture having enhanced, synergistic stabilizing properties is described as well.Type: GrantFiled: October 1, 1998Date of Patent: January 30, 2001Assignee: The United States of America as represented by the Secretary of the ArmyInventors: Chares S. Leveritt, Steven W. Bunte, Eugene F. Rothgery, Carl G. Seefried, Nathan Klein
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Patent number: 6140537Abstract: A method of producing a boron-based compound represented by general formula (1) including a first step of reacting lithium, magnesium or a compound containing lithium, a compound represented by general formula (2), and a compound represented by general formula (3): R.sup.2 --Y to produce a borate metal salt represented by general formula (4), and a second step of adding to the borate metal salt an onium halide represented by general formula (5): Z.sup.+ .multidot.X.sup.- to effect ion exchange reaction (the symbols in the formulae have the same meanings as described in the specification).According to the production method of the present invention, a high purity boron-based compound represented by the general formula (1) above useful as a photopolymerization initiator and a light-absorbing decolorizing agent can be obtained in a short time and a high yield as compared with the conventional method.Type: GrantFiled: August 5, 1999Date of Patent: October 31, 2000Assignee: Showa Denko K.K.Inventors: Tsuyoshi Katoh, Morihiko Yamada
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Patent number: 6093826Abstract: A method for preparing C(5)-substituted 1,2-dihydro-5H-chromeno[3,4-.function.]quinolines from a lactol precursor is provided. The method comprises converting the lactol to one of a select number of mixed acetal derivatives, and then treating the acetals with a Grignard reagent. The new process provides products in higher yield and greater purity. Novel intermediates of this method are also claimed.Type: GrantFiled: June 8, 1998Date of Patent: July 25, 2000Assignee: Ligand Pharmaceuticals IncorporatedInventors: James P. Edwards, Todd K. Jones
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Patent number: 6090950Abstract: Novel chiral boron and aluminum hydride complexes, compositions comprising the chiral hydride complexes, and methods for their synthesis and use are described. The novel chiral hydride complexes are of the formulas:MBH.sub.4-n-a (R*).sub.n (R').sub.a ;MBH.sub.2-b (R**) (R').sub.b ;MBH(R***);MBH(R*) (R");MAlH.sub.4-n-a (R*).sub.n (R').sub.a ;MAlH.sub.2-b (R**)(R').sub.b ;MAlH(R***); andMAlH(R*) (R"),whereinM is Na.sup.+, Li.sup.+ or K.sup.+ ;each R* is independently a monodentate chiral ligand;R** is a bidentate chiral ligand;R*** is a tridentate chiral ligand;R' is a monodentate achiral ligand;R" is a bidentate achiral ligand;n is 1-3;a is 0-2; andb is 0-1,with the proviso that n+a.ltoreq.3, and with the further proviso that when R** is S-BINOL, M is not Li.sup.+.Type: GrantFiled: August 23, 1996Date of Patent: July 18, 2000Assignee: Zeeland Chemicals, Inc.Inventor: Glenn L. Heise
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Patent number: 6083903Abstract: Disclosed herein are boronic ester and acid compounds, their synthesis and uses. More specifically, disclosed herein is a method for reducing the rate of degradation of proteins in an animal comprising contacting cells of the animal with certain boronic ester and acid compounds.Type: GrantFiled: May 16, 1995Date of Patent: July 4, 2000Assignee: LeukoSite, Inc.Inventors: Julian Adams, Yu-Ting Ma, Ross Stein, Matthew Baevsky, Louis Grenier, Louis Plamondon
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Patent number: 6071895Abstract: The present invention discloses the compounds of general formula (1) ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 are optionally substituted carbonyl and amide derivatives which are useful as inhibitors of retroviral proteases, and are effective in treating conditions characterized by unwanted activity of these enzymes, such as acquired immume deficiency syndrome.Type: GrantFiled: February 22, 1999Date of Patent: June 6, 2000Assignee: Narhex LimitedInventor: Damian Wojciech Grobelny
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Patent number: 6066730Abstract: Disclosed herein is a method for reducing the rate of degradation of proteins in an animal comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.Type: GrantFiled: May 26, 1998Date of Patent: May 23, 2000Assignee: ProScript, Inc.Inventors: Julian Adams, Yu-Ting Ma, Ross Stein, Matthew Baevsky, Louis Grenier, Louis Plamondon
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Patent number: 6060462Abstract: This invention relates to electrophilic dipeptide analogs conjugated to an N,N-disubstituted .alpha.-amino acid as inhibitors of trypsin-like serine protease enzymes.Type: GrantFiled: August 1, 1997Date of Patent: May 9, 2000Assignee: DuPont Pharmaceuticals CompanyInventors: Robert Anthony Galemmo, Jr., Matthew Mark Abelman, Eugene Cruz Amparo, John Matthew Fevig, Robert Madara Knabb, William Henry Miller, Gregory James Pacofsky, Patricia Carol Weber, Joseph Cacciola
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Patent number: 6037505Abstract: The anantoselective borane reduction of prochiral ketones to optically pure alcohols is effectively achieved by performing the reduction in the precence of catalytic amounts of the new and valuable oxazaborolidine compounds of formulas (I) and (II). The compounds of formulas (I) and (II) may be isolated and purified prior to use in the reduction reactions or the compounds of formulas (I) and (II) may be generated in situ.Type: GrantFiled: April 26, 1999Date of Patent: March 14, 2000Assignee: Pfizer Inc.Inventor: George Joseph Quallich
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Patent number: 6008353Abstract: Compounds of formula (I) or pesticidally acceptable salts thereof, compositions containing them and methods of use.Type: GrantFiled: October 7, 1997Date of Patent: December 28, 1999Assignee: Rhone-Poulenc Inc.Inventor: Tai-Teh Wu
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Patent number: 6002044Abstract: A method for producing a borate compound represented by formula (1) is disclosed, comprising a first step of reacting lithium or magnesium or a compound containing lithium or magnesium, a halide represented by formula (2) and a compound represented by formula (3) in a solvent to produce a boronate compound precursor, a second step of reacting lithium or magnesium or a compound containing lithium or magnesium, a halide represented by formula (4) and the boronate compound precursor obtained in the first step in a solvent to produce a borate metal salt, and a third step of adding an onium halide represented by formula (5) to the borate metal salt obtained in the second step to effect ion-exchange reaction (the formulae are as described in the specification).Type: GrantFiled: November 10, 1998Date of Patent: December 14, 1999Assignee: Showa Denko K.K.Inventors: Morihiko Yamada, Tsuyoshi Katoh, Norihide Arai
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Patent number: 5917045Abstract: A class of predominantly hydrophilic 1,8-naphthalimide dyes. The dye contains at least two 1,8-naphthalimide ring systems, joined by a spacer moiety. Each of the 1,8-naphthalimide ring system has a ring nitrogen atom and bears, at the 4 position, an amino nitrogen atom, carrying a hydrogen. The remaining unsatisfied valences, if present, of the ring nitrogen atoms or the amino nitrogen atoms, or all, are occupied by one or more alkyl substituents. Each of the 1,8-naphthalimide ring system is free of an azo substituent and is also free of a nucleofuge. Upon activation by an activating agent in an environment independent of the presence or absence of oxygen, these compounds generate activated species. The activated species can cause structural changes in lipid and any associated proteins and polypeptides, extra- or intra-cellular or transmembrane, leading to polymerization and crosslinking.Type: GrantFiled: June 7, 1995Date of Patent: June 29, 1999Assignee: MicroBioMed CorporationInventors: David E. Lewis, Ronald E. Utecht, Millard M. Judy, J. Lester Matthews
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Patent number: 5864044Abstract: Disclosed herein are novel trisulfonated phathalocyanines, processes for making them and their derivatives. Also disclosed are key intermediates consisting of Boron(III) subphathalocyanines. Further disclosed are novel uses for various water soluble trisulfophathalocyanines, trisulfobenzonapthoporphyrazines and trisulfonated phathalocyanines. The new uses are directed to photsensitizers for the photodynamic therapy of cancer, the inactivation of viruses in stored blood, organic semiconductors, disk memory material or as materials for gas sensors. In the compounds of the present invention, the central metal atom may be Zn, Co(II), Ni or Cu(II).Type: GrantFiled: July 24, 1997Date of Patent: January 26, 1999Assignee: Universite de SherbrookeInventors: Johannes E. Van Lier, Svetlana V. Kudrevich, Sandra Gilbert
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Patent number: 5852191Abstract: Boron complexes of certain bis-heterocyclic compounds are provided. The complexes resemble monomethine cyanines and are useful for imparting fluorescent properties to materials by covalent and noncovalent association. The compounds have the following general formula: ##STR1## wherein the dotted lines Z.sub.1 and Z.sub.2 represent the atoms necessary to complete a structure selected from the group consisting of one ring, two fused rings, and three fused rings, each said ring having five or six atoms, and each said ring comprising carbon atoms and, optionally, no more than two atoms selected from oxygen, nitrogen and sulfur, and R.sub.1 through R.sub.5 represent various atoms or groups and M is Cl or F.Type: GrantFiled: June 7, 1995Date of Patent: December 22, 1998Assignee: Carnegie Mellon UniversityInventors: Bhalchandra M. Karandikar, Alan S. Waggoner, Ratnakar B. Mujumdar
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Patent number: 5808070Abstract: A process is disclosed for preparing a compound of the FormulaM (R.sup.1 R.sup.2 N.BH.sub.3)or a complex thereof of the FormulaM (R.sup.1 R.sup.2 N.BH.sub.3).xLwhereinM is Li, Na, K, Rb or Cs;R.sup.1 is H, an aliphatic C.sub.1 to C.sub.5 residue, an aromatic residue, or a cycloaliphatic residue;R.sup.2 is H, an aliphatic C.sub.1 to C.sub.5 residue, an aromatic residue, or a cycloaliphatic residue; orR.sup.1 and R.sup.2 form a common cyclic residue;L is a dipolar aprotic solvent; andx is a numerical value from 0.1 to 5, which comprises the steps of:(a) where the compound of the Formula M(R.sup.1 R.sup.2 N.BH.sub.3) is prepared, reacting a compound of the FormulaR.sup.1 R.sup.2 NH.BH.sub.3with an alkali metal or an alkali metal amide in a non-polar aliphatic or aromatic solvent; or(b) where the complex of the Formula M(R.sup.1 R.sup.2 N.BH.sub.3).xL is prepared, reacting the compound of the FormulaR.sup.1 R.sup.2 NH.BH.sub.Type: GrantFiled: June 25, 1997Date of Patent: September 15, 1998Assignee: Metallgesellschaft AktiengesellschaftInventors: Heinrich Noth, Steffen Thomas, Peter Rittmeyer, Ulrich Wietelmann
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Patent number: 5731439Abstract: The present invention relates generally to .alpha.-aminoboronic acids and corresponding peptide analogs in which the .alpha.-carbon is substituted with an optionally functionalized piperidine containing alkyl group. These compounds are useful as inhibitors of trypsin-like serine protease enzymes.Type: GrantFiled: March 24, 1995Date of Patent: March 24, 1998Assignee: The DuPont Merck Pharmaceutical CompanyInventors: David John Carini, Joseph Cacciola, Celia Dominguez, John Matthew Fevig
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Patent number: 5702952Abstract: The invention provides novel labelled boronic acid conjugates of formula ##STR1## (wherein V is a reporter moiety; W.sup.2 is a bond or an organic linker moiety;W.sup.1 is a *SO.sub.2 NR.sup.2, *CONR.sup.2 or *CH.sub.2 N.sup..sym. R.sup.2.sub.2 group bound at the *-marked atom to the phenyl ring;R.sup.1 is hydrogen or an electron withdrawing substituent group; andeach R.sup.2 independently is hydrogen or an optionally hydroxylated and optionally C.sub.1-6 -alkoxylated C.sub.1-6 -alkyl group) and salts thereof, e.g. for use in assays for cis-diols such as glycated blood proteins, having enhanced water-solubility and storage stability.Type: GrantFiled: February 21, 1997Date of Patent: December 30, 1997Assignee: Axis Biochemicals ASAInventors: Erling Sundrehagen, Frank Frantzen
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Patent number: 5686608Abstract: A process for preparing polycyclic aromatic compounds by cross-coupling aromatic boron compounds with aromatic halogen compounds or perfluoroalkylsulfonates in the presence of metallic palladium as catalyst comprises adding to the reactiona) at least one water-soluble complexing ligand andb) sufficient water for the reaction mixture to form an aqueous phase.The reaction of the invention proceeds chemoselectively so that even electrophilic groups such as esters or nitriles do not have an adverse effect on the course of the reaction.The use according to the invention of a water-soluble complexing ligand in an aqueous phase enables polycyclic aromatic compounds to be prepared in very good yields and at the same time very high purity, in particular without contamination by the complexing ligands.Type: GrantFiled: April 24, 1995Date of Patent: November 11, 1997Assignee: Hoechst AktiengesellschaftInventors: Steffen Haber, Javier Manero
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Patent number: 5679818Abstract: The present invention is a compound having the formula:R.sup.1 --Ac.sup.1 --Ar.sup.1 --M--Ar.sup.2 --Ac.sup.2 --R.sup.2where R.sup.1 and R.sup.2 are independently selected from the group consing of hydrogen, unsubstituted alkyl groups, substituted alkyl groups, unsubstituted aryl groups, and substituted aryl groups, where Ac.sup.1 and Ac.sup.2 are independently selected alkynyl groups having at least 1 carbon-carbon triple bond, where Ar.sup.1 and Ar.sup.2 are independently selected substituted or unsubstituted aromatic diradicals, and where M has the structure ##STR1## where m is a positive integer, wherein x, p, y, r, n, and z are independently selected integers, where z.noteq.0 when n.noteq.0, and where R.sup.3 through R.sup.14 are independently selected from the group consisting of hydrogen, unsubstituted alkyl groups, substituted alkyl groups, unsubstituted aryl groups, and substituted aryl groups.Type: GrantFiled: July 26, 1996Date of Patent: October 21, 1997Assignee: The United States of America as represented by the Secretary of the NavyInventors: Daniel Bucca, Teddy M. Keller
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Patent number: 5646172Abstract: Novel imidazoles of the formula ##STR1## wherein the substituents are as defined in the disclosure and their non-toxic, pharmaceutically acceptable addition salts with acids and bases having antiandrogenic activity.Type: GrantFiled: September 7, 1995Date of Patent: July 8, 1997Assignee: Roussel UclafInventors: Andre Claussner, Francois Goubet, Jean-Georges Teutsch
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Patent number: 5646098Abstract: The invention relates to novel compositions comprising ene and free radical adducts of unsaturated and saturated hydrocarbons, and acyclic and cyclic vicinal polycarbonyl compounds such as diethyl ketomalonate and indantrione. The adducts are reacted with nucleophiles such as amines, electrophiles such as anhydrides and esters, and metal ions. Post-products are obtained via reaction of said products with capping reagents such as boric acid. Compositions containing said adducts, products and post-products include oleaginous substances such as fuels and lube oils.Type: GrantFiled: May 13, 1994Date of Patent: July 8, 1997Assignee: Exxon Chemical Patents IncInventor: Stanley J. Brois
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Patent number: 5639739Abstract: The present invention relates generally to .alpha.-aminoboronic acids and corresponding peptide analogs of the formula (I): ##STR1## in which the .alpha.-carbon is substituted with an optionally functionalized imidazole containing alkyl group. These compounds are useful as inhibitors of trypsin-like serine protease enzymes, especially thrombin, Factor X and Factor VII.Type: GrantFiled: March 24, 1995Date of Patent: June 17, 1997Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Celia Dominguez, Joseph Cacciola, John Matthew Fevig
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Patent number: 5631364Abstract: The invention provides novel labelled boronic acid conjugates of formula ##STR1## (wherein V is a reporter moiety; W.sup.2 is a bond or an organic linker moiety;W.sup.1 is a *SO.sub.2 NR.sup.2, *CON.sup.2 or *CH.sub.2 N.sym.R.sup.2 .sub.2 group bound at the *-marked atom to the phenyl ring;R.sup.1 is hydrogen or an electron withdrawing substituent group; andeach R.sup.2 independently is hydrogen or an optionally hydroxylated and optionally C.sub.1-6 -alkoxylated C.sub.1-6 -alkyl group) and salts thereof, e.g. for use in assays for cis-diols such as glycated blood proteins, having enhanced water-solubility and storage stability.Type: GrantFiled: March 31, 1994Date of Patent: May 20, 1997Assignee: AXIS Biochemicals ASAInventors: Erling Sundrehagen, Frank Frantzen
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Patent number: 5629428Abstract: 3-Chloropyridines, process for their preparation, and their use in liquid-crystal mixturesA 3-chloropyridine of the formula (I) ##STR1## in which the symbols have the following meaning: R.sup.1 and R.sup.2, independently of one another, are, for example, H or straight-chain or branched alkyl, A.sup.1, A.sup.2, A.sup.3 and A.sup.4 are identical or different and are, for example, 1,4-phenylene, pyrazine-2,5-diyl or trans-1,4-cyclohexylene, M.sup.1, M.sup.2, M.sup.3 and M.sup.4 are identical or different and are, for example, --O-- or --CO--O--, R.sup.3, R.sup.4, R.sup.6 and R.sup.7, independently of one another are, for example, H or straight-chain or branched alkyl, M.sup.5 is, for example, --O--CO-- or a single bond, k, l, m, n, o, p, q and r are zero or one, with the proviso that the sum k+m+p+r is less than 4 and greater than zero, can advantageously be employed as a component in ferroelectric liquid-crystal mixtures.Type: GrantFiled: May 10, 1994Date of Patent: May 13, 1997Assignee: Hoechst AktiengesellschaftInventors: Hubert Schlosser, Dietmar Jungbauer, Javier Manero
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Patent number: 5597922Abstract: Methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions and inducing anesthesia are disclosed by administering to an animal in need of such treatment a compound which has high binding to the glycine receptor.Type: GrantFiled: July 29, 1994Date of Patent: January 28, 1997Assignees: State of Oregon, Acting by and through the Oregon State Board of Higher Education, Acting for and on Behalf of the Oregon Health Sciences University and the University of Oregon, Acea Pharmaceuticals, Inc., The Regents of the University of CaliforniaInventors: Sui X. Cai, John F. W. Keana, Eckard Weber
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Patent number: 5591726Abstract: The present invention provides heterocyclylalkyl diarylboron ester and thioester compounds of formula I ##STR1## and their use for the prevention, control or amelioration of diseases caused by fungi. Further provided are compositions and methods comprising those compounds for the protection of plants from fungal infection and disease.Type: GrantFiled: September 26, 1994Date of Patent: January 7, 1997Assignee: American Cyanamid CompanyInventors: Bomi P. Patel, Henry Van Tuyl Cotter, Jerome M. Lavanish
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Patent number: 5585390Abstract: Compounds of the general formula: ##STR1## wherein m, X, Y, A, R.sub.2 and R.sub.3 are defined in the description, and medicaments containing the same.Type: GrantFiled: May 9, 1995Date of Patent: December 17, 1996Assignee: Adir Et CompagnieInventors: Muriel Duflos, Sylvie Robert-Piessard, Lucien Welin, Guillaume Le Baut, Daniel-Henri Caignard, Pierre Renard, G erard Adam
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Patent number: 5574049Abstract: 2,2-di(C.sub.1-5 alkyl)- and trans-2,2-di(C.sub.1-5 alkyl)-3,4-dihydro-3-hydroxy-6-(pyridin-4-yl)-2H-1-benzopyrans, e.g. of formula ##STR1## in which R.sub.1 and R.sub.2 =H, alkyl, hydroxyalkyl or alkoxyalkyl, at least one being other than H, R.sub.3 =typically a 2-piperidinone group, R.sub.4 =H and R.sub.5 =--OH or R.sub.4 +R.sub.5 =an additional bond, and R.sub.6, R.sub.7 are alkyl and R.sub.8 is H or alkyl, and N-oxides, esters and salts thereof, processes for their production and their uses as pharmaceuticals e.g. as K.sup.+ -channel openers, bronchodilators and asthma prophylactic agents.Type: GrantFiled: June 6, 1995Date of Patent: November 12, 1996Assignee: Sandoz Ltd.Inventor: Paul W. Manley
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Patent number: 5563127Abstract: Novel boronic acid and ester and carboxyl-modified amino acid compounds of the Formula I, which are inhibitors of trypsin-like enzymes, are disclosed :R.sup.1 --Z--CHR.sup.2 --A,where R.sup.1, Z, R.sup.2 and A are defined within.Type: GrantFiled: December 27, 1994Date of Patent: October 8, 1996Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Eugene C. Amparo, William H. Miller, Gregory J. Pacofsky, John Wityak, Patricia C. Weber, John J. V. Duncia, Joseph B. Santella, III
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Patent number: 5552548Abstract: The borane reduction of prochiral ketones to optically pure alcohols is effectively achieved by the utilization of catalytic amounts of the new and valuable oxazaborolidine catalysts of formula (I).Type: GrantFiled: October 13, 1994Date of Patent: September 3, 1996Assignee: Pfizer Inc.Inventor: George J. Quallich
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Patent number: 5516909Abstract: A method for producing amine-boranes, specifically pyridine-borane which is highly stable and of good color is described.Type: GrantFiled: February 15, 1994Date of Patent: May 14, 1996Assignee: Boulder Scientific CompanyInventor: Jeffrey M. Sullivan
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Patent number: RE36115Abstract: A method for producing amine-boranes, specifically pyridine-borane which is highly stable and of good color is described.Type: GrantFiled: February 14, 1997Date of Patent: February 23, 1999Assignee: Boulder Scientific CompanyInventor: Jeffrey M. Sullivan